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Vactosertib Hydrochloride

Catalog No. T15262   CAS 1352610-25-3
Synonyms: TEW-7197 Hydrochloride, EW-7197 Hydrochloride

Vactosertib Hydrochloride is an orally active and ATP-competitive ALK5 inhibitor (IC50: 12.9 nM). It has potently antimetastatic activity and anticancer effect. Vactosertib Hydrochloride also inhibits ALK2 and ALK4 (IC50: 17.3 nM).

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Vactosertib Hydrochloride Chemical Structure
Vactosertib Hydrochloride, CAS 1352610-25-3
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2 mg 5 days $ 67.00
5 mg 5 days $ 128.00
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Biological Description
Chemical Properties
Storage & Solubility Information
Description Vactosertib Hydrochloride is an orally active and ATP-competitive ALK5 inhibitor (IC50: 12.9 nM). It has potently antimetastatic activity and anticancer effect. Vactosertib Hydrochloride also inhibits ALK2 and ALK4 (IC50: 17.3 nM).
Targets&IC50 ALK5:12.9 nM
In vitro Vactosertib inhibits the TGFβ-induced nuclear translocation of Smad2/3 in 4T1 cells and MCF10A cells (IC50: 10-30 nM for Vactosertib on pSmad3 in 4T1 cells). Vactosertib (10-1000 nM; 30 minutes; 4T1 cells) treatment blocks the TGFβ-induced phosphorylation of Smad2 or Smad3 in a dose-dependent manner in 4T1 cells. Vactosertib abrogates TGFb1-induced tumor cell migration and invasion. Moreover, Vactosertib abolishes the TGFβ1-induced effects on genes related to epithelial-to-mesenchymal transition (EMT) [1].
In vivo Vactosertib inhibits the epithelial-to-mesenchymal transition (EMT) in both TGFβ-treated breast cancer cells and 4T1 orthotopic-grafted mice. Vactosertib (40 mg/kg; i.p.; every other day; for 10 weeks; MMTV/c-Neu female mice) treatment inhibits Smad/TGFβ signaling, cell migration, invasion, and lung metastasis in MMTV/c-Neu mice. Vactosertib enhances cytotoxic T lymphocyte activity in 4T1 orthotopic-grafted mice and increased the survival time of 4T1-Luc and 4T1 breast tumor-bearing mice [1].
Synonyms TEW-7197 Hydrochloride, EW-7197 Hydrochloride
Molecular Weight 435.89
Formula C22H19ClFN7
CAS No. 1352610-25-3

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

H2O: 50 mg/mL (114.71 mM), sonification is recommended.

DMSO: 50 mg/mL (114.71 mM), sonification is recommended.

TargetMolReferences and Literature

1. Son JY, et al. EW-7197, a novel ALK-5 kinase inhibitor, potently inhibits breast to lung metastasis. Mol Cancer Ther. 2014 Jul;13(7):1704-16. 2. Naka K, et al. Novel oral transforming growth factor-β signaling inhibitor EW-7197 eradicates CML-initiating cells. Cancer Sci. 2016 Feb;107(2):140-8.

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Keywords

Vactosertib Hydrochloride 1352610-25-3 Angiogenesis Tyrosine Kinase/Adaptors ALK EW 7197 Hydrochloride TEW-7197 Hydrochloride EW7197 Hydrochloride TEW 7197 Hydrochloride EW-7197 Hydrochloride TEW7197 Hydrochloride inhibitor inhibit

 

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